The present invention relates to antibacterial agents of the cephalosporin class in which the six membered ting of the cephalosporin nucleus is substituted with an aryl or heteroaryl group at position three.
Cephoxitin was an early cephalosporin antibacterial agent having a broad spectrum; it has the following formula: ##STR3##
The cephalosporins of the present invention have activity against gram positive and gram negative microorganisms, and are believed to be useful against methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS). The antibacterial compounds of the present invention thus comprise an important contribution to therapy for these difficult to control pathogens.
Moreover, there is an increasing need for agents effective against such pathogens (MRSA/MRCNS) which are at the same time relatively free from undesirable side effects. And, the current agent of choice, vancomycin, a glycopeptide antibacterial, is experiencing an ever increasing amount of resistance in the MRSA/MRCNS pathogens.